Fluconazole is an important member of the azole class of antifungal agents, as it is orally active and has low toxicity, but its extensive use has resulted in emergence of fluconazole-resistant fungal strains. It is therefore necessary to develop analogues of fluconazole effective against resistant strains, and research in this direction has resulted in many new compounds containing fluconazole pharmacophores. However, to address the issues like toxicity, solubility, cost, broad spectrum of activity etc, it is necessary to develop superior antifungal agents. The structure-activity relationship studies have shown that presence of one triazole ring, halogenated phenyl ring and tertiary alcoholic oxygen functionality is necessary for antifungal activity of fluconazole or its analogues.
Some of the recent references describing synthesis and antifungal activity of fluconazole analogues are described in the following articles: Borate et al. Bioorg. Med. Chem. Lett. 21 (16), 4873-8 (2011); Borate et al. Bioorg. Med. Chem. Lett. 20, 722 (2010); Pore et al. Bioorg. Med. Chem. Lett. 19, 759 (2009); Konosu et al. Bioorg. Med. Chem. Lett. 19, 2013 (2009); Bioorg. Med. Chem. 16, 7055 (2008); Bioorg. Med. Chem. Lett. 18, 3261 (2008); Bioorg. Med. Chem. Lett. 18, 6538 (2008); Bioorg. Med. Chem. Lett. 17 (13), 3686 (2007).
WO 2012047762 discloses antifungal agents for treating infections by microorganism, wherein said antifungal agent comprises an antifungal compound containing triazole, imidazole or echinocandin moieties, linked to another antifungal or immunosuppressive compound, via a covalently-bonded linker. Thus, said PCT application teaches connecting of two active moieties via a linking moiety to obtain enhanced antifungal activity, whereas the present invention discloses coupling of one active moiety to another inactive moiety for obtaining compounds with enhanced antifungal activity.
771/DEL/2008 discloses new class of antifungal drugs for obtaining better antifungal spectrum, containing 1,2,3-triazol-1-yl or 4-yl moieties optionally substituted with bile acid or (long) alkyl chains, to obtain better antifungal spectrum, however said application does not cover antifungal compounds of present invention.
WO 2012123952 discloses enantiomers of fluconazole analogues containing thieno-[2,3-d]pyrimidin-4(3H)-one moiety as antifungal agents which are depicted as follows in formula A and formula B.

Thus, from the aforementioned prior art, it is clear that there is still a need in the art to provide novel compounds containing fluconazole pharmacophores with superior antifungal activity, and methods for preparations thereof.